Synthesis and Anticholinesterase Evaluation of Cassine, Spectaline and Analogues

Autor:	Marcela C. R. Silva, Adriana F. L. Vilela, Carmen L. Cardoso, Ronaldo A. Pilli
Jazyk:	angličtina
Rok vydání:	2022
Předmět:	cassine spectaline synthesis analogues anticholinesterase activity Pharmacy and materia medica RS1-441
Zdroj:	Scientia Pharmaceutica, Vol 90, Iss 4, p 63 (2022)
Druh dokumentu:	article
ISSN:	2218-0532 0036-8709
DOI:	10.3390/scipharm90040063
Popis:	In this work, twelve analogues of piperidine alkaloids (-)-cassine and (-)-spectaline were synthesized, as well as the racemic forms of these natural products. The compounds were evaluated for their inhibition of electric eel acetylcholinesterase (AChEee) and human butyrylcholinesterase (BChEhu) by on-flow mass-spectrometry-based dual-enzyme assay, and the inhibition mechanisms for the most potent analogues were also determined. Our results showed a preference for BChEhu inhibition with compounds 10c (Ki = 5.24 μM), 12b (Ki = 17.4 μM), 13a (Ki = 13.2 μM) and 3 (Ki = 11.3 μM) displaying the best inhibitory activities.
Databáze:	Directory of Open Access Journals
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